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CAS No.: 905586-69-8

AZ960 Catalog No. CSN17120

Synonyms: AZ 960

AZ 960 is a potent ATP-competitive JAK inhibitor with IC50 values of <3 nM and 9nM for JAK2 and JAK3, respectively.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 JAK2

IC50:3nM
描述The Janus-associated kinase (Jak) family, comprised 4 different protein-tyrosine kinases, Jak1, Jak2, Jak3, and TYK2, plays an important role in cellular survival, proliferation, and differentiation. Jak kinases are key mediators of signaling downstream of a variety of cytokine and/or growth factor receptors. Each Jak possesses kinase domain, a catalytically inactive pseudokinase, and amini-terminal, ezrin, radixin, and moesin (FERM). Cytokine receptors bind to FERM domain, leading to activation of Jaks, which create docking sites for members of signal transducers and activators of transcription (Stat) family, including Stat3 and Stat5. AZ960 is a potent and selective ATP competitive inhibitor of the Jak2 kinase with a K_i of 0.45 nM. AZ960 was also shown to be active against other kinases, including TrkA, Aurora-A, and FAK, with IC₅₀ of around 0.1 μM. In a vitro study, HTLV-1 (human T-cell lymphotropic virus type 1) - infected T cells cells were incubated with AZ960 (0.3 or 1 μM) for 2 days and the result showed that AZ960 suppressed the growth of MT-1 and MT-2 cells with IC₅₀ of 0.8 and 1 μM. Intact GV-oocytes were cultured with CEP-33779 for 12 h to inhibit JAK2 activity during maturation. The result showed that a large proportion of the CEP-33779 treated oocytes failed to extrude polar body I, only 21.14 ± 4.03% (n=382) of these oocytes reached the M II stage after 12 h in vitro maturation, a rate significantly lower than that of non-treated control oocytes (81.44±3.64%, n=357)^[3]. HTLV-1-infected T cells and MOLT-4 cells (5 × 10⁵ cells/mL) were cultured with various concentrations of AZ960 (0.03-1 μM) for 2 days. AZ960 inhibited the growth of freshly isolated ATL (Adult T-cell leukemia/lymphoma) cells in a dose-dependent manner with IC₅₀ of 0.3 μM, and AZ960 also inhibited the growth of MOLT-4 cells in a dose-dependent manner with IC₅₀ of 1.2 μM, which indicated blockade of Jak2/Stats by Jak2 kinase inhibitor AZ960 represents a promising treatment strategy for individuals with ATL.
作用机制AZ 960 binds to the ATP-binding site of JAK2 kinase.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02178956	Gastric Cancer ... more >> Gastroesophageal Junction Cancer Collapse <<	Phase 3	Active, not recruiting	June 2019	-
NCT01689519	Malignant Melanoma	Phase 3	Active, not recruiting	December 28, 2019	-
NCT02908672	Melanoma	Phase 3	Active, not recruiting	July 29, 2023	-

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参考文献

[1] Yang J, Ikezoe T, et al. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010 Dec;9(12):3386-95.
[2] Gozgit JM, Bebernitz G, et al. Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J Biol Chem. 2008 Nov 21;283(47):32334-43.
[3] Yang J, Ikezoe T, Nishioka C, Furihata M, Yokoyama A. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010 Dec;9(12):3386-95. doi: 10.1158/1535-7163.MCT-10-0416. PMID: 21159615.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8220 mL
- 14.1101 mL
- 28.2202 mL
- 5 mM
- 0.5644 mL
- 2.8220 mL
- 5.6440 mL
- 10 mM
- 0.2822 mL
- 1.4110 mL
- 2.8220 mL

技术信息

CAS号

905586-69-8

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H16F2N6

运输

蓝冰

分子量

354.36

别名

AZ 960

溶解度

DMSO	71.0 mg/mL (200.4 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (8.5 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02178956	Gastric Cancer ... more >> Gastroesophageal Junction Cancer Collapse <<	Phase 3	Active, not recruiting	June 2019	-
NCT01689519	Malignant Melanoma	Phase 3	Active, not recruiting	December 28, 2019	-
NCT02908672	Melanoma	Phase 3	Active, not recruiting	July 29, 2023	-
NCT01307397	Malignant Melanoma	Phase 3	Completed	-	-
NCT02291289	Colorectal Cancer	Phase 2	Suspended(Following iDMC revie... more >>w of cohort 4 data a temporary recruitment halt to the whole study and a temporary halt to randomisation into cohort 4 has been undertaken) Collapse <<	December 29, 2021	-
NCT01307397	-	-	Completed	-	-
NCT01667419	Melanoma	Phase 3	Active, not recruiting	October 14, 2020	-
NCT01689519	-	-	Active, not recruiting	-	-
NCT01667419	-	-	Active, not recruiting	-	-
NCT02768207	Metastatic Melanoma	Phase 2	Active, not recruiting	July 30, 2019	Belgium ... more >> UZ Brussel Brussel, Belgium, 1090 Institut Jules Bordet Bruxelles, Belgium, 1000 CHIREC Edith Cavell Bruxelles, Belgium, 1180 UZ Antwerpen Edegem, Belgium, 2650 UZ Gent Gent, Belgium, 9000 Jessa Zkh (Campus Virga Jesse) Hasselt, Belgium, 3500 AZ Groeninge Kortrijk, Belgium, 8500 Clinique Ste-Elisabeth Namur, Belgium, 5000 AZ Delta (Campus Wilgenstraat) Roeselare, Belgium, 8800 AZ Nikolaas (Sint Niklaas) Sint Niklaas, Belgium, 9100 Sint Augustinus Wilrijk Wilrijk, Belgium, 2610 Poland Centrum Onkologii Instytut Klinika Nowotworow Ukladowych i Uogolnionych Krakow, Poland Szpital Kliniczny im. Heliodora Święcickiego UM w Poznaniu. Poznań, Poland, 60-355 Centrum Onkologii- Instytut; im. M.Skłodowskiej-Curie Warszawa, Poland, 02-781 Collapse <<

AZ960 Catalog No. CSN17120

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